Glycopeptide antibacterials

Judice JK, Pace JL. (2003) Semi-synthetic glycopeptide antibacterials. 

Barrett JF. Recent developments in glycopeptide antibacterials. Curr Opin Investig Drugs. 2005 6 781-790. 

Macrocyclic peptides as antibacterial glycopeptide antibiotics 98KGS1605. 

Bleomycin is a complex of no less than 16 glycopeptide antibiotics made from the family Streptomyces verticilus, which have different R groups [88-94]. Bleomycines exhibit antitumor, antiviral, and antibacterial activity. When bound to DNA, they disturb the spiraling of both single and double strands of DNA. To a lesser degree, they inhibit RNA and protein synthesis. It is administered both intravenously and intramuscularly. 

Teicoplanin is a glycopeptide antibiotic that is very similar to vancomycin in mechanism of action and antibacterial spectrum. Unlike vancomycin, it can be given intramuscularly as well as intravenously. Teicoplanin has a long half-life (45-70 hours), permitting once-daily dosing. This drug is available in Europe but has not been approved for use in the United States. 

The majority of these are antibiotics and they cover a diverse group including the glycopeptide, avoparcin (95), tetracycline, macrolides, such as tylosin (23) and virginiamycin (96), as well as peptides, glycopeptides and terpenes. Antibacterials such as the quinoxaline-1,4-dioxide, carbadox (39), and nitrofurans, e.g. furazolidone (35) and nitrovin (97), are also represented. 

Septicemias - [ANTIBIOTICS - GLYCOPEPTIDES (DALBAHEPTIDES)] (Vol 2) - [ANTIBACTERIAL AGENTS SYNTHETIC - SULFONAMIDES] (Vol 2)... 

Cooper RDG, Snyder NJ, Zweifel MJ et al (1996) Reductive alkylation of glycopeptide antibiotics synthesis and antibacterial activity. J Antibiot 49 575-581... 

NJ Snyder, RD Cooper, BS Briggs, M Zmijewski, DL Mullen, RE Kaiser, TI Nicas. Enzymatic deacylation of teicoplanin followed by reductive alkylation synthesis and antibacterial activity of new glycopeptides. J Antibiot 51 945-951, 1998. 

Hoffmann, R Bulet, P Urge, L and Otvos, L., Jr. (1999) Range of activity and metabolic stability of synthetic antibacterial glycopeptides from insects. Biochim. Biophys. Acta 1426,459 167. 

Singh MP et al (2003) Mannopeptimycins, new cyclic glycopeptide antibiotics produced by Streptomyces hygroscopicus LL-AC98 antibacterial and mechanistic activities. Antimicrob Agents Ch 47 62-69... 

Motiei L et al (2009) Antibacterial cyclic D,L-alpha-glycopeptides. Chem Commun 3693-3695... 

The type-V glycopeptide antibiotics with complestatin or chloropeptin as representatives show no antibacterial activity. Instead, the inhibition of binding of viral glycoprotein gpl20 to cellular CD4-receptors was found. Characteristic features for this subclass are a DE-biaryl ring, which is formed by 4-hydroxyphenylglycine (AA4) and tryptophan (AA2). 

Finally, it has to be noted that glycopeptides only represent one option to combat infections by gram-positive bacteria. Current research is focused on other cell wall biosynthesis inhibitors (e.g., (3-lactams, cephalosporins) or even on the development of antibacterial agents (e.g., tetracyclines, ketohdes, and quinolone antibiotics) against other targets.An important drug candidate in this context is hnezolid (Zyvox), which is an entirely synthetic oxazolidinone antibiotic with in vitro and in vivo efficiency against MRS A and VRE. ... 

Bucaneve G, Menichetti F, Del Favero A. Cost analysis of 2 empiric antibacterial regimens containing glycopeptides for the treatment of febrile neutropenia in patients with acute leukaemia. Pharmacoeconomics 1999 15(l) 85-95. 

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